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Cressier D., Dhilly M., Cao Pham T. T., Fillesoye F., Gourand F., Maiza A., Martins A. F., Morfin J.-F., Geraldes C. F. G. C., Toth E. and Barre L.

Gallium-68 Complexes Conjugated to Pittsburgh Compound B : Radiolabeling and Biological Evaluation

Molecular Imaging and Biology (2016) 18 (3) 334-343

par Frapart - publié le

Abstract :

PURPOSE : The aim of this work is to develop an efficient and fully automated radiosynthesis of three derivatives of the Pittsburgh compound B labeled with gallium-68 for the detection of amyloid plaques.
PROCEDURES : The radiolabeling of the precursors and purification of the radiolabeled agents by high pressure liquid chromatography has been studied prior to their in vitro and in vivo evaluations.
RESULTS : The complete process led, in 50 min, to pure Ga-68 products in a 12-38 % yield and with appreciable specific radioactivity (SRA, 85-168 GBq/mumol) which enabled us to demonstrate a considerable in vivo stability of the products. Unfortunately, this result was associated with a poor blood-brain barrier (BBB) permeability and a limited uptake of our compounds by amyloid deposits was observed by in vitro autoradiography.
CONCLUSION : Although we have not yet identified a compound able to significantly mark cerebral amyloidosis, this present investigation will likely contribute to the development of more successful Ga-68 radiotracers.